[EN] ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'ÉTHYNYLE A TITRE DE MODULATEURS DU RÉCEPTEUR MÉTABOTROPIQUE DU GLUTAMATE
申请人:HOFFMANN LA ROCHE
公开号:WO2017009275A1
公开(公告)日:2017-01-19
The present invention relates to compounds of formula I wherein R1 is lower alkyl; R2 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; n is 0, 1 or 2; V/U are independently from each other O or CH2, wherein V and U cannot be simultaneously O; L is a five or six membered heteroaryl group, selected from or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
本发明涉及式I的化合物,其中R1为较低的烷基;R2为苯基或吡啶基,吡啶基中的N原子可能位于不同位置;n为0、1或2;V/U分别为O或CH2,其中V和U不能同时为O;L为选自五元或六元杂环芳基团的杂环芳基团,选择自药用盐或酸加盐,对于外消旋混合物,或对应的对映体和/或光学异构体和/或立体异构体。这些化合物可用于治疗帕金森病、焦虑症、呕吐、强迫症、自闭症、神经保护、癌症、抑郁症和2型糖尿病。